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Home - Products - GPCR/G Protein - Somatostatin Receptor - L-803087

L-803087

CAS No. 217480-26-7

L-803087( —— )

Catalog No. M32990 CAS No. 217480-26-7

L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    L-803087
  • Note
    Research use only, not for human use.
  • Brief Description
    L-803087 is a potent and selective agonist of the growth inhibitor sst4 receptor with a Ki value of 0.7 nM for sst4, demonstrating over 280-fold selectivity compared to other growth inhibitory receptors.
  • Description
    L-803087 is a potent and selective somatostatin sst4 receptor agonist with a Ki of 0.7 nM. L-803087 is >280-fold higher than other somatostatin receptors. L-803087 facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice.
  • In Vitro
    L-803087 has Ki values for cloned human sst1, sst2, sst3 and sst5 receptors of 199, 4720, 1280 and 3880 nM, respectively.L-803087 has a diamine moiety that maps to lysine on the phmacophore, but relation of this molecule to the aromatic and the Trp substituents of the phmacophore are not obvious. L-803087 does not inhibit secretion of growth hormone, insulin, or glucagon.
  • In Vivo
    L-803087 (5 nmol) is doubled seizure activity in wild-type mice on average. Interestingly, this effect is blocked by 3 nmol Octreotide. In hippocampal slices from wild-type mice, Octreotide (2 μM) does not modify AMPA-mediated synaptic responses while facilitation occurred with L-803087 (2 μM).
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Somatostatin Receptor
  • Recptor
    Somatostatin
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    217480-26-7
  • Formula Weight
    485.53
  • Molecular Formula
    C25H29F2N5O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 250 mg/mL (514.90 mM; Ultrasonic )
  • SMILES
    COC(=O)[C@H](CCCNC(N)=N)NC(=O)CCCc1c([nH]c2c(F)cc(F)cc12)-c1ccccc1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Rohrer SP, et al. Rapid identification of subtype-selective agonists of the somatostatin receptor through combinatorial chemistry. Science. 1998 Oct 23;282(5389):737-40.?
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